排序方式: 共有31条查询结果,搜索用时 31 毫秒
1.
Giorgio Roma Aldo Ermili Alessandro Balbi Elda Massa Mario Di Braccio 《Journal of heterocyclic chemistry》1981,18(8):1619-1623
The reaction of 3-(dimethylamino)-1-oxo-1H-naphtho[2,1-b]pyran-2-carbaldehyde (Ia) with o-phenylenediamines or N-monosubstituted o-phenylenediamines in refluxing glacial acetic acid afforded the corresponding naphtho[1′,2′:5,6]pyrano[2,3-b][1,5]benzodiazepin-15-(8H)ones V in very good yields. A similar result was achieved when the reaction was carried out in refluxing pyridine, using N-monosubstituted o-phenylenediamine hydrochlorides. The isolation of a significant intermediate as well as the synthesis through a different univocal pathway confirmed the structure of the compounds V. Moreover the reaction of Ia with N-monosubstituted o-phenylenediamines in refluxing pyridine generally afforded only low yields of compounds V, sometimes together with naphtho[1′,2′:5,6]pyrano[2,3-b][1,5]benzodiazepin-15-(13H)ones VII, isomers of V. 相似文献
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Susana Araceli Carrizales Álvarez Anna Ilyina Karla Monzerratt Gregorio Jáuregui José Luis Martínez Hernández Brenda Berenice Vazquez Gutiérrez Elda Patricia Segura Ceniceros Alejandro Zugasti Cruz Hened Saade Caballero Raúl Guillermo López Campos 《Applied biochemistry and biotechnology》2014,174(5):1945-1958
Avian influenza viruses preferentially bind to sialic acid alpha-2,3-galactose (N-SA-α-2,3-Gal) receptors on epithelial cells. Herein, we describe a procedure we have developed for isolation of N-SA-α-2,3-Gal receptors from porcine trachea using magnetic nanoparticles (NPs) coated with chitosan (NP-Ch) and functionalized with Maackia amurensis lectin (NP-lectin). Magnetic nanoparticles were coated with chitosan in a one-step co-precipitation, and then M. amurensis lectin was immobilized covalently using glutaraldehyde. Lectin coated nanoparticles were incubated with sialic acid enriched fraction of tracheal homogenate, and N-SA-α-2,3-Gal receptor was extracted under magnetic field in two cycles. The presence of 66.4 kDa protein was determined by sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE). The interaction of immobilized receptor (NP-Ch-R) with M. amurensis lectin (NP-Ch-R-L) was demonstrated by Fourier transform infrared spectrometry (FTIR) and thermogravimetric analysis (TGA). 相似文献
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Francesca Al Francesca Miraglia Alessandro Orticoni Elda Judica Maria Cotelli Paolo Maria Rossini Fabrizio Vecchio 《Entropy (Basel, Switzerland)》2020,22(11)
Human brain, a dynamic complex system, can be studied with different approaches, including linear and nonlinear ones. One of the nonlinear approaches widely used in electroencephalographic (EEG) analyses is the entropy, the measurement of disorder in a system. The present study investigates brain networks applying approximate entropy (ApEn) measure for assessing the hemispheric EEG differences; reproducibility and stability of ApEn data across separate recording sessions were evaluated. Twenty healthy adult volunteers were submitted to eyes-closed resting EEG recordings, for 80 recordings. Significant differences in the occipital region, with higher values of entropy in the left hemisphere than in the right one, show that the hemispheres become active with different intensities according to the performed function. Besides, the present methodology proved to be reproducible and stable, when carried out on relatively brief EEG epochs but also at a 1-week distance in a group of 36 subjects. Nonlinear approaches represent an interesting probe to study the dynamics of brain networks. ApEn technique might provide more insight into the pathophysiological processes underlying age-related brain disconnection as well as for monitoring the impact of pharmacological and rehabilitation treatments. 相似文献
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Lara Bianchi Giovanni Petrillo Egon Rizzato Elda Severi Marco Stenta Cinzia Tavani 《Tetrahedron》2009,65(1):336-757
(1E,3Z)-1-Aryl-4-methanesulfonyl-2-nitro-1,3-butadienes (8), derived from the initial ring-opening of 3-nitrothiophene (5), have been found to undergo a facile base-induced cyclization leading to thiopyran S,S-dioxides (9), thus furnishing a further example of effective ring-enlargement from 5- to 6-membered sulfur heterocycles. Compounds 9 are obtained as single racemic mixtures in satisfactory yields; they still contain a nitrovinylic moiety, which can be exploited for further modifications targeted to new derivatives endowed with either synthetic or pharmacological potentialities e.g., in the field of L-type Ca2+-channel blockers. 相似文献
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Frego L Gautschi E Martin L Davidson W 《Rapid communications in mass spectrometry : RCM》2006,20(16):2478-2482
Recently, a hydrogen/deuterium exchange method termed SUPREX (Stability of Unpurified Proteins from Rates of hydrogen/deuterium EXchange), capable of measuring protein/ligand binding constants, which utilizes matrix-assisted laser desorption/ionization mass spectrometry (MALDI-MS), has been reported. Unlike more conventional approaches, SUPREX is inherently capable of measuring Kd values of tight binding ligands. Here we present a SUPREX-based method, incorporating automation and electrospray ionization (ESI)-MS, to measure Kd values for very potent inhibitors of the kinase PKCtheta. The use of ESI offers an alternative to MALDI, with the advantages of improved mass measurement precision for larger proteins, and amenability to automation. Kd values generated by this method are in good agreement with those generated by a molecular protein kinase assay. 相似文献
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Bianchi L Dell'Erba C Maccagno M Petrillo G Rizzato E Sancassan F Severi E Tavani C 《The Journal of organic chemistry》2005,70(22):8734-8738
[reaction: see text] In prosecution of previous work on the thermal cyclization of 1-aryl-4-methanesulfonyl-2-nitro-3-phenylsulfonyl-1,3-butadienes (7), the 3-unsubstituted derivatives 8, deriving from the initial ring opening of 3-nitrothiophene (2), have been likewise found herein to undergo cyclization, followed by aromatization, in analogous mild experimental conditions, leading to the ring-fused homo- or heteroaromatic nitro derivatives 10. The concerted electrocyclic nature of the process is strongly supported by the outcome of tests based on the variation of the polarity of the solvent or of the electron density on the aryl of 8. Thus, the successful application of the process to the non-phenylsulfonyl-activated 8 significantly widens the scope of a synthetically valuable overall ring-opening/ring-closing procedure from nitrothiophenes. Support to the recently renewed interest in thermal 6pi electrocyclizations as a tool for the construction of the benzene ring is furthermore provided. 相似文献
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Elda Markovic Kim Nguyen Stephen Clarke Kristina Constantopoulos Janis Matisons George P. Simon 《Journal of polymer science. Part A, Polymer chemistry》2013,51(23):5038-5045
A series of polyurethane hybrid networks have been synthesized using octakis(m‐isoprenyl‐α,α′‐dimethylbenzylisocyanato dimethylsiloxy) octasilsesquioxane (Q8M8TMI) as a crosslinking agent. The formation of the urethane linkages within the polyurethane hybrids was confirmed by photoacoustic FTIR spectroscopy. The TGA and DSC studies demonstrated that the incorporation of the POSS crosslinking agents altered the thermal properties of the polyurethanes, and that this was dependent on the length of the polyethylene glycol chain. © 2013 Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. 2013 , 51, 5038–5045 相似文献
9.
Synthesis and pharmacological properties of azido derivatives of 1,5-benzothiazepine Ca antagonist 总被引:1,自引:0,他引:1
H Narita M Gaino T Suzuki H Kurosawa H Inoue T Nagao 《Chemical & pharmaceutical bulletin》1990,38(2):407-410
Since azido derivatives of 1,5-benzothiazepine Ca antagonist available for photoaffinity labeling are required for further studies of voltage-sensitive Ca channels, we synthesized 3-(p-azidobenzoyloxydeacetyl)- and 3-(4-azidobutyryloxydeacetyl)-diltiazem, and studied their pharmacological properties. Both azido compounds showed similar relaxing actions to diltiazem in K(+)-depolarized dog arteries. They also showed a similar increasing action to diltiazem, but less potent, on the coronary and vertebral blood flow in the anesthetized dog. Moreover, their negative inotropic effects in the guinea pig papillary muscle were similar to or slightly more potent than that of diltiazem under physiological conditions, but were less potent when studied in K+ depolarizing solution. A radioligand binding study in rat skeletal muscle microsomes revealed that the azido derivatives had similar properties to diltiazem, but the nonspecific binding of 3-(p-azidobenzoyloxydeacetyl)-diltiazem was too high to allow estimation of its KD and Bmax values. In conclusion, we synthesized azido derivatives of diltiazem which were considered to share a common binding site on the voltage-dependent Ca channel with diltiazem in skeletal muscle microsomes and in vascular smooth muscle. 相似文献
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Lara Bianchi Massimo Maccagno Marino Novi Egon Rizzato Elda Severi Cinzia Tavani 《Tetrahedron》2004,60(23):4967-4973
The (E)-2-aryl-1-[2-(methylthio)phenyl]-1-nitroethylenes 5 can easily be oxidized to the relevant sulfones 6 and effectively subjected to cyclization via an intramolecular Michael addition after metallation with lithium bis(trimethylsilyl)amide in THF. After quenching with ammonium chloride the 3-aryl-4-nitrothiochroman S,S-dioxides 2 are obtained as diastereomeric mixtures in good to excellent yields. Both yields and stereochemistry of the ring-closure step appear to be influenced by steric effects of the 3-aryl moiety. As sulfides 5 derive from an initial ring opening of 3-nitrobenzo[b]thiophene (1), the overall 1 to 2 process can be considered as an effective 5 to 6 ring enlargement of the sulfur heterocycle. A conformational 1H NMR and molecular-mechanics investigation on the isolated diastereomeric 2 has also been accomplished. 相似文献